Table 1.
IC50 values of the tested compounds 5a–k and 8a–h against human aldose reductase.
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Comp. | R | AR inhibition, IC50 (μM) |
5a | 4-NO2 | 0.22 |
5b | 4-Cl | 0.46 |
5c | 4-Br | 0.49 |
5d | 4-F | 0.57 |
5e | 4-CH3 | 0.55 |
5f | 4-OCH3 | 0.28 |
5g | 3,4,5-triOCH3 | 0.72 |
5h | 3-NO2 | 0.51 |
5k | 3-Br | 0.41 |
8a | 4-NO2 | 1.98 |
8b | 4-Cl | 0.16 |
8c | 4-Br | 0.21 |
8d | 4-F | 0.33 |
8e | 4-CH3 | 0.29 |
8f | 4-OCH3 | 0.94 |
8g | 3,4,5-triOCH3 | 0.27 |
8h | 3,4-diOCH3 | 0.45 |
Epalrestat | – | 0.10 |